NZ771435B2 - Methods of treating conditions related to the S1P1 receptor - Google Patents
Methods of treating conditions related to the S1P1 receptor Download PDFInfo
- Publication number
- NZ771435B2 NZ771435B2 NZ771435A NZ77143516A NZ771435B2 NZ 771435 B2 NZ771435 B2 NZ 771435B2 NZ 771435 A NZ771435 A NZ 771435A NZ 77143516 A NZ77143516 A NZ 77143516A NZ 771435 B2 NZ771435 B2 NZ 771435B2
- Authority
- NZ
- New Zealand
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- medicament
- formulated
- Prior art date
Links
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 title 1
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 title 1
- 229940125904 compound 1 Drugs 0.000 claims abstract 18
- 150000003839 salts Chemical class 0.000 claims abstract 14
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims abstract 12
- 239000012453 solvate Substances 0.000 claims abstract 8
- 206010012438 Dermatitis atopic Diseases 0.000 claims abstract 2
- 201000008937 atopic dermatitis Diseases 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims 11
- 125000002059 L-arginyl group Chemical class O=C([*])[C@](N([H])[H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=N[H])N([H])[H] 0.000 claims 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 159000000007 calcium salts Chemical class 0.000 claims 2
- 239000002775 capsule Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- -1 tetrahydrocyclopenta[b]indolyl Chemical group 0.000 claims 1
- MVGWUTBTXDYMND-QGZVFWFLSA-N 2-[(3r)-7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid Chemical compound C([C@@H]1CC(=O)O)CC(C2=C3)=C1NC2=CC=C3OCC(C=C1C(F)(F)F)=CC=C1C1CCCC1 MVGWUTBTXDYMND-QGZVFWFLSA-N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- DUYSYHSSBDVJSM-KRWOKUGFSA-N sphingosine 1-phosphate Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)COP(O)(O)=O DUYSYHSSBDVJSM-KRWOKUGFSA-N 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
Abstract
Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S lP1) receptor-associated disorder comprising prescribing and/or administering to an individual with atopic dermatitis in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1 ,2, 3,4-tetrahydrocyclopenta[ b ]indol-3-yl)acetic acid ( Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in an amount equivalent to about 1.5 to about 2.5 mg of compound 1.
Claims (18)
1. Use of (R)(7-(4-cyclopentyl(trifluoromethyl)benzyloxy)-1,2,3,4- 5 tetrahydrocyclopenta[b]indolyl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in the manufacture of a medicament to treat atopic dermatitis in an individual in need thereof, wherein the medicament is formulated to deliver Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof in an amount equivalent to about 2.0 mg.
2. The use of claim 1, wherein the medicament is formulated to deliver Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in an amount equivalent to 2.0 mg of Compound 1. 15
3. The use of claim 1 or claim 2, wherein the medicament is formulated for daily administration.
4. The use of any one of claims 1 to 3, wherein the medicament is formulated for oral administration. 20
5. The use of any one of claims 1 to 4, wherein the medicament is formulated as a capsule or tablet suitable for oral administration.
6. The use of any one of claims 1 to 5, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is selected from: 25 Compound 1; a calcium salt of Compound 1; and an L-arginine salt of Compound 1.
7. The use of any one of claims 1 to 6, wherein the Compound 1, or a pharmaceutically acceptable 30 salt, hydrate, or solvate thereof, is an L-arginine salt of Compound 1.
8. The use of any one of claims 1 to 7, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is an anhydrous, non-solvated crystalline form of an L-arginine salt of Compound 1.
9. The use of any one of claims 1 to 6, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is an anhydrous, non-solvated crystalline form of Compound 1.
10. The use of claim 1, wherein the medicament is formulated to deliver Compound 1, or a pharmaceutically acceptable salt thereof, in an amount equivalent to about 2.0 mg of
Compound 1. 5 11. The use of claim 1, wherein the medicament is formulated to deliver Compound 1, or a pharmaceutically acceptable salt thereof, in an amount equivalent to 2.0 mg of Compound 1.
12. The use of claim 10 or claim 11, wherein the medicament is formulated for daily administration.
13. The use of any one of claims 10 to 12, wherein the medicament is formulated for oral administration.
14. The use of any one of claims 10 to 13, wherein the medicament is formulated as a capsule or 15 tablet suitable for oral administration.
15. The use of any one of claims 10 to 14, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is selected from: Compound 1; 20 a calcium salt of Compound 1; and an L-arginine salt of Compound 1.
16. The use of any one of claims 10 to 15, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is an L-arginine salt of Compound 1.
17. The use of any one of claims 10 to 16, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is an anhydrous, non-solvated crystalline form of an L-arginine salt of Compound 1. 30
18. The use of any one of claims 10 to 15, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is an anhydrous, non-solvated crystalline form of Compound 1.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562100362P | 2015-01-06 | 2015-01-06 | |
| US201562159550P | 2015-05-11 | 2015-05-11 | |
| NZ734220A NZ734220A (en) | 2015-01-06 | 2016-01-06 | Methods of treating conditions related to the s1p1 receptor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NZ771435A NZ771435A (en) | 2024-08-30 |
| NZ771435B2 true NZ771435B2 (en) | 2024-12-03 |
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